Molecular recognition of protein kinase binding pockets for design of potent and selective kinase inhibitors
JJL Liao - Journal of medicinal chemistry, 2007 - ACS Publications
Protein kinases constitute one of the largest protein families in humans. 1, 2 The kinase
enzymes in this family catalyze phosphorylation of serine, threonine, or tyrosine residues …
enzymes in this family catalyze phosphorylation of serine, threonine, or tyrosine residues …
The many faces of H89: a review
A Lochner, JA Moolman - Cardiovascular drug reviews, 2006 - Wiley Online Library
ABSTRACT H89 is marketed as a selective and potent inhibitor of protein kinase A (PKA).
Since its discovery, it has been used extensively for evaluation of the role of PKA in the …
Since its discovery, it has been used extensively for evaluation of the role of PKA in the …
Hematopoietic progenitor kinase 1 in tumor immunology: a medicinal chemistry perspective
Q Zhu, N Chen, X Tian, Y Zhou, QD You… - Journal of Medicinal …, 2022 - ACS Publications
Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-restricted member of the
serine/threonine Ste20-related protein kinases, is a negative regulator of the T cell receptor …
serine/threonine Ste20-related protein kinases, is a negative regulator of the T cell receptor …
[HTML][HTML] Structural basis of constitutive activity and a unique nucleotide binding mode of human Pim-1 kinase
Pim-1 kinase is a member of a distinct class of serine/threonine kinases consisting of Pim-1,
Pim-2, and Pim-3. Pim kinases are highly homologous to one another and share a unique …
Pim-2, and Pim-3. Pim kinases are highly homologous to one another and share a unique …
Measuring and interpreting the selectivity of protein kinase inhibitors
LA Smyth, I Collins - Journal of chemical biology, 2009 - Springer
Protein kinase inhibitors are a well-established class of clinically useful drugs, particularly
for the treatment of cancer. Achieving inhibitor selectivity for particular protein kinases often …
for the treatment of cancer. Achieving inhibitor selectivity for particular protein kinases often …
The crystal structures of TrkA and TrkB suggest key regions for achieving selective inhibition
T Bertrand, M Kothe, J Liu, A Dupuy, A Rak… - Journal of molecular …, 2012 - Elsevier
The Trk family of neurotrophin receptors, which includes the three highly homologous
proteins TrkA, TrkB and TrkC, is strongly associated with central and peripheral nervous …
proteins TrkA, TrkB and TrkC, is strongly associated with central and peripheral nervous …
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity
BG Szczepankiewicz, C Kosogof… - Journal of medicinal …, 2006 - ACS Publications
The c-Jun N-terminal kinases (JNK-1,-2, and-3) are members of the mitogen activated
protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines …
protein (MAP) kinase family of enzymes. They are activated in response to certain cytokines …
Heterocycles in breast cancer treatment: the use of pyrazole derivatives
S Ardevines, E Marqués-López… - Current Medicinal …, 2023 - ingentaconnect.com
Among the aromatic heterocycle rings, pyrazole–a five-membered ring with two adjacent
nitrogen atoms in its structure has been postulated as a potent candidate in the …
nitrogen atoms in its structure has been postulated as a potent candidate in the …
Insights into current tropomyosin receptor kinase (TRK) inhibitors: development and clinical application
The use of kinase-directed precision medicine has been heavily pursued since the
discovery and development of imatinib. Annually, it is estimated that around∼ 20 000 new …
discovery and development of imatinib. Annually, it is estimated that around∼ 20 000 new …
Design, synthesis and antitumor activity of novel pyrazolo [3, 4-d] pyrimidine derivatives as EGFR-TK inhibitors
MA Abdelgawad, RB Bakr, OA Alkhoja… - Bioorganic chemistry, 2016 - Elsevier
Abstract A novel series of 2-(3, 6-dimethyl-1-phenyl-1H-pyrazolo [3, 4-d] pyrimidin-4-yloxy)-
N-(4-substitutedbenzylidene) acetohydrazide (12a–g) was prepared and their structures …
N-(4-substitutedbenzylidene) acetohydrazide (12a–g) was prepared and their structures …